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Last Updated: March 28, 2024

Claims for Patent: 5,462,740


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Summary for Patent: 5,462,740
Title: Rectally-administered, epileptic-seizure-inhibiting composition
Abstract:This invention provides a rectally administered composition for inhibiting epileptic seizure and to its methods of use. The composition contains, in a suitable solvent, an anti-epileptic agent for inhibiting epileptic seizure, a buffer for maintaining pH, and a thickener for imparting a viscosity to the composition effective for rectal administration by injection to a patient in epileptic seizure.
Inventor(s): Evenstad; Kenneth L. (Wayzata, MN), O'Neill; Victoria A. (Wayzata, MN), Gorham; Thomas R. (Brooklyn Park, MN)
Assignee: Athena Neurosciences, Inc. (San Francisco, CA)
Application Number:08/122,685
Patent Claims: 1. A viscous, epileptic-seizure-inhibiting composition comprising:

(a) about 0.1-2.5 wt-% of the total composition of an anti-epileptic agent;

(b) a buffer system in an amount effective to maintain the pH of the composition at about 5.5-7.5;

(c) about 1-10 wt-% of a cellulose ether thickener to impart a viscosity to the composition so that it is suitable for administration by rectal injection to a human patient; and

(d) about 25-95 wt-% solvent.

2. The composition of claim 1 wherein the anti-epileptic agent is selected from the group consisting of barbiturates, benzodiazepines, dipropylacetic acid derivatives, hydantoins, oxazolidinediones and succinimides.

3. The composition of claim 2 wherein the anti-epileptic agent is diazepam.

4. The composition of claim 1 wherein the amount of the cellulose ether thickener is effective to impart an apparent viscosity of about 1,000 to about 8,000 cps to the composition.

5. The composition of claim 1 wherein the cellulose ether thickener is selected from the group consisting of methyl cellulose, carboxylmethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose.

6. The composition of claim 5 wherein the cellulose ether thickener is hydroxypropyl methylcellulose.

7. The composition of claim 1 wherein the solvent is water or water and a water-miscible organic solvent in an amount effective to inhibit precipitation of the anti-epileptic agent from the composition.

8. A viscous, epileptic-seizure-inhibiting composition comprising:

(a) about 0.25-0.75 wt-% diazepam;

(b) a buffer system in an amount effective to maintain the pH of the composition at about 5.5-7.5;

(c) about 1-10 wt-% cellulose ether thickener;

(d) about 25-75 wt-% of a non-toxic water-miscible organic solvent; and

(e) the balance, water.

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